2-(ethoxymethyl)-tropane derivatives are valuable pharmaceutical active substances for the treatment of various central nervous disorders, such as, e.g., Parkinson's or Alzheimer's disease.
According to the teaching of International Publication No. WO9730997, which is incorporated by reference herein in its entirety, 2-(ethoxymethyl)-tropane derivatives are prepared either from a 2-(tosylmethyl)-tropane derivative by reacting with ethoxide, or by reacting a 2-(hydroxymethyl)-tropane derivative with sodium hydride as base and diethylsulphate. For safety reasons, production on an industrial scale using sodium hydride is virtually impossible. Moreover, this ethoxylation is not really reproducible, the reaction times are long, and the active substance is produced in unsatisfactory yields as a solid, which is difficult to isolate.
Thus, an object underlying the present invention is to provide a process that enables 2-(ethoxymethyl)-tropane derivatives to be produced in good yields on a large industrial scale, while avoiding the disadvantages that occur with the processes known from the prior art.